Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369891 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
A series of lactam sulfonamides has been discovered and optimized as inhibitors of the Kv1.5 potassium ion channel for treatment of atrial fibrillation. In vitro structure–activity relationships from lead structure C to optimized structure 3y are described. Compound 3y was evaluated in a rabbit PD-model and was found to selectively prolong the atrial effective refractory period at submicromolar concentrations.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Roine I. Olsson, Ingemar Jacobson, Tommy Iliefski, Jonas Boström, Öjvind Davidsson, Ola Fjellström, Annika Björe, Christina Olsson, Johan Sundell, Ulrik Gran, Jonna Gyll, Jesper Malmberg, Olle Hidestål, Hans Emtenäs, Tor Svensson, Zhong-Qing Yuan,